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Application of A-cyclo trihydroxy substituted pentacyclic triterpene compounds in pharmaceuticals

A technology of pentacyclic triterpenes and trihydroxyl groups is applied in the application field of preparing antibacterial or anti-tobacco mosaic virus medicines, and can solve the problems that the research on anti-phytopathogenic bacteria and anti-tobacco mosaic virus has not been reported before.

Active Publication Date: 2016-12-07
THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the research on the anti-phytopathogenic bacteria and anti-tobacco mosaic virus of this type of compound has never been reported.

Method used

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  • Application of A-cyclo trihydroxy substituted pentacyclic triterpene compounds in pharmaceuticals
  • Application of A-cyclo trihydroxy substituted pentacyclic triterpene compounds in pharmaceuticals
  • Application of A-cyclo trihydroxy substituted pentacyclic triterpene compounds in pharmaceuticals

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0163] Embodiment 1 of the present invention: take any one of compound I17, U2, U4, A2, A3, add appropriate amount of starch and microcrystalline cellulose according to the pharmaceutical method, and mix well, mix the hydroxymethyl cellulose solution with the above-mentioned Mix the powder, pass through an 80-mesh sieve to obtain wet granules, dry at 50-60°C, sieve carboxymethyl starch salt, magnesium stearate and talc in advance, and then add them to the above-mentioned granules and press into tablets to obtain tablets . The preparation is taken orally, twice a day, and the dosage for each dose is 5-30 mg calculated as the raw material. For the treatment of infectious diseases caused by Staphylococcus aureus such as purulent infection, pneumonia, pseudomembranous colitis, pericarditis, etc.

Embodiment 2

[0164] Embodiment 2: Take any one of compounds I3, I15, I18, I23, U1, U3, U5, A4, add appropriate amount of sodium citrate, polyethylene glycol, distilled water according to the pharmaceutical method, mix well and fully dissolve, adjust The pH value of the solution is 7.5-8.5 and then filtered, and the concentration of the raw material is 1 mg / ml, which is divided into 2 ml per ampoule and sterilized to obtain the injection. The preparation is used for injection, twice a day, and the amount of each injection is 5-30 mg based on the raw material drug. For the treatment of infectious diseases caused by Staphylococcus aureus.

Embodiment 3

[0165] Example 3: Take any one of compounds Ia, Ic, Ij, Io, Ip, I13, A1, A5, and A7, pulverize it through an 80-mesh sieve, add an appropriate amount of vegetable oil containing 10% beeswax according to the pharmaceutical method, and mix well ; Prepare capsule material with gelatin:glycerol:distilled water:preservative=1:0.4:0.8:0.003, add the mixture of the aforementioned compound and vegetable oil, and press to obtain a soft capsule. The preparation is taken orally, twice a day, and the dosage for each dose is 5-30 mg calculated as the raw material. For the treatment of infectious diseases caused by Staphylococcus aureus.

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Abstract

The invention discloses an application of A-cyclo trihydroxy substituted pentacyclic triterpene compounds in preparation of drugs resistant to tobacco mosaic viruses. The general formula of the compounds is as follows, wherein hydroxyl of C1, C2 and C3 are respectively alpha or beta configuration; R1 and R2 are selected form hydrogen or methyl and R1 is different from R2; R3 is selected from -COOH, -CH2OH, -CHO, -COOR<1>, -CONH2, -CONHR<1> and CONR<1>R<2>; R<1> and R<2> are selected from alkyls of 1-15 carbon atom, substituted or unsubstituted phenyl and substituted or unsubstituted alkyl benzene; a substituted group is selected from halogen, hydroxyl, cyan, amidogen, nitro, sulfydryl or phenyl, acyl, aryl, alkoxy and alkyl containing 1-15 carbons. The compounds have quite high activity in resisting the tobacco mosaic viruses, and good application prospect in the field of pesticides is achieved.

Description

[0001] This application is a divisional application for an invention patent application with an application date of April 28, 2014, an application number of 2014101738959, and the title of "Application of A-ring trihydroxy-substituted pentacyclic triterpenoids in pharmaceuticals". technical field [0002] The invention relates to the application of A-ring trihydroxy-substituted pentacyclic triterpenoid compounds in pharmacy, in particular to the application in preparing antibacterial or anti-tobacco mosaic virus medicaments, and belongs to the technical field of medicinal uses of compounds. Background technique [0003] Pentacyclic triterpenoids are widely distributed in nature, and they have a variety of biological activities, including antitumor, antibacterial, antiviral, antihypertensive, hypoglycemic, etc. (Dzubak Petr, Hajduch Marian, Vydra David. et al. Pharmacological activities of natural triterpenoids and their therapeuticimplications. Nat. Prod. Rep., 2006, 23, 394–...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A01N37/36A01N31/04A01N35/02A01P1/00
CPCA01N31/04A01N35/02A01N37/36
Inventor 杨小生黄丽荣骆衡史亚男郝小江
Owner THE KEY LAB OF CHEM FOR NATURAL PROD OF GUIZHOU PROVINCE & CHINESE ACADEMY OF SCI
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